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https://www.readbyqxmd.com/read/27906404/highly-efficient-and-stable-mos2-fets-with-reversible-n-doping-using-a-dehydrated-poly-vinyl-alcohol-coating
#1
César J Lockhart de la Rosa, Amirhasan Nourbakhsh, Markus Heyne, Inge Asselberghs, Cedric Huyghebaert, Iuliana Radu, Marc Heyns, Stefan De Gendt
Despite rapid progress in 2D molybdenum disulfide (MoS2) research in recent years, MoS2 field-effect transistors (FETs) still suffer from a high metal-to-MoS2 contact resistance and low intrinsic mobility, which are major hindrances to their future application. We report an efficient technique to dope thin-film MoS2 FETs using a poly(vinyl-alcohol) (PVA) polymeric coating. This results in a reduction of the contact resistance by up to 30% as well as a reduction in the channel resistance to 20 kΩ sq(-1). Using a dehydration process, we were able to effectively control the surface interactions between MoS2 and the more electropositive hydroxyl groups (-OH) of PVA, which provided a controllable and yet reversible increase in the charge carrier density to a value of 8...
December 1, 2016: Nanoscale
https://www.readbyqxmd.com/read/27905605/an-efficient-2d-11-b-11-b-solid-state-nmr-spectroscopy-strategy-for-monitoring-covalent-self-assembly-of-boronic-acid-derived-compounds-the-transformation-and-unique-architecture-of-bortezomib-molecules-in-the-solid-state
#2
J Brus, J Czernek, M Urbanova, L Kobera, A Jegorov
The difficulty in the prediction of the complicated solid-state structure of boronic acid derivatives, resulting from the complex pathway of reversible covalent interactions, represents a significant obstacle to the development of a new generation of advanced supramolecular systems such as covalent organic frameworks of efficient anticancer drugs. In this contribution, various 2D (11)B-(11)B solid-state NMR correlation techniques supported by DFT calculations were explored to formulate a reliable tool for monitoring the covalent assembly of boronic acid residues in the solid state...
December 1, 2016: Physical Chemistry Chemical Physics: PCCP
https://www.readbyqxmd.com/read/27905163/fungal-glycolipid-hydrolase-inhibitors-and-their-effect-on-cryptococcus-neoformans
#3
Andres Gonzalez Santana, Christina Tysoe, Guanggan Hu, James Kronstad, Ethan Goddard-Borger, Stephen Withers
Pathogenic fungi kill an estimated 1.3 million people each year. This number is predicted to rise as drug resistance spreads, thus antifungal drugs with novel modes of action are urgently required. Fungal endoglycoceramidase-related proteins 1 and 2 (EGCrP-1 and -2), which hydrolyse glucosylceramide and ergosteryl beta-glucoside, respectively, are important for fungal cell growth and have been identified as potential targets for drug development. A library of iminosugar derivatives was screened against EGCrP-1 and -2, thereby identifying a number of competitive inhibitors with nanomolar affinities...
November 30, 2016: Chembiochem: a European Journal of Chemical Biology
https://www.readbyqxmd.com/read/27904965/chitosan-hydrogel-microspheres-an-effective-covalent-matrix-for-crosslinking-of-soluble-dextranase-to-increase-stability-and-recycling-efficiency
#4
Faiza Shahid, Afsheen Aman, Muhammad Asif Nawaz, Asad Karim, Shah Ali Ul Qader
Dextranase is a unique biocatalyst that has high specificity and stereo-selectivity towards a complex biopolymer known as dextran. Dextranase has wide industrial application, but most of the time harsh environmental conditions adversely affect the functionality and stability of the enzyme. To overcome this issue, a covalent cross-linking immobilization method was adapted in the current study utilizing a nontoxic and biocompatible matrix known as chitosan. Chitosan hydrogel microspheres were synthesized using chitosan which exhibited noteworthy physical and mechanical strength...
November 30, 2016: Bioprocess and Biosystems Engineering
https://www.readbyqxmd.com/read/27904766/the-role-of-pim1-in-the-ibrutinib-resistant-abc-subtype-of-diffuse-large-b-cell-lymphoma
#5
Hsu-Ping Kuo, Scott A Ezell, Sidney Hsieh, Karl J Schweighofer, Leo Wk Cheung, Shiquan Wu, Mutiah Apatira, Mint Sirisawad, Karl Eckert, Yu Liang, Jeff Hsu, Chun-Te Chen, Darrin Beaupre, Betty Y Chang
Diffuse large B cell lymphoma (DLBCL) is a heterogeneous lymphoma and the most common subtype of non-Hodgkin lymphoma, accounting for roughly 30% of newly diagnosed cases in the United States. DLBCL can be separated into the activated B cell-like (ABC) and germinal center B cell-like (GCB) subtypes, with distinct gene expression profiles, oncogenic aberrations, and clinical outcomes. ABC-DLBCL is characterized by chronically active B-cell receptor (BCR) signaling that can be modulated by Bruton's tyrosine kinase (BTK) activity...
2016: American Journal of Cancer Research
https://www.readbyqxmd.com/read/27904094/design-and-synthesis-of-functional-molecules-based-on-complexation-and-their-biological-applications
#6
Yosuke Hisamatsu
 In this review, we introduce the development of supermolecules, host-guest complexes, and metal complexes formed from the combination of non-covalent interactions and/or coordination bonds, as well as their biological applications. An adenine selective host molecule 1 provides a correctly oriented array of complementary hydrogen bonding sites for the adenine nucleobase. Furthermore, the new DDAA (D: hydrogen bond donor, A: hydrogen bond acceptor) module 4 and ADDA module 7 have been developed as quadruple hydrogen-bonding modules...
2016: Yakugaku Zasshi: Journal of the Pharmaceutical Society of Japan
https://www.readbyqxmd.com/read/27903679/the-bruton-s-tyrosine-kinase-btk-inhibitor-acalabrutinib-demonstrates-potent-on-target-effects-and-efficacy-in-two-mouse-models-of-chronic-lymphocytic-leukemia
#7
Sarah E M Herman, Arnau Montraveta, Carsten U Niemann, Helena Mora-Jensen, Michael Gulrajani, Fanny Krantz, Rose Mantel, Lisa L Smith, Fabienne McClanahan, Bonnie Harrington, Dolors Colomer, Todd Covey, John C Byrd, Raquel Izumi, Allard Kaptein, Roger Ulrich, Amy Johnson, Brian J Lannutti, Adrian Wiestner, Jennifer A Woyach
PURPOSE: Acalabrutinib (ACP-196) is a novel, potent, and highly selective BTK inhibitor, which binds covalently to Cys481 in the ATP-binding pocket of BTK. We sought to evaluate the anti-tumor effects of acalabrutinib treatment in two established mouse models of chronic lymphocytic leukemia (CLL). EXPERIMENTAL DESIGN: Two distinct mouse models were used, the TCL1 adoptive transfer model where leukemic cells from Eμ-TCL1 transgenic mice are transplanted into C57BL/6 mice, and the human NSG primary CLL xenograft model...
November 30, 2016: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/27903430/minimizing-the-risk-of-chemically-reactive-metabolite-formation-of-new-drug-candidates-implications-for-preclinical-drug-design
#8
Andreas Brink, Axel Pähler, Christoph Funk, Franz Schuler, Simone Schadt
Many pharmaceutical companies aim to reduce reactive metabolite formation by chemical modification at early stages of drug discovery. A practice often applied is the detection of stable trapping products of electrophilic intermediates with nucleophilic trapping reagents to guide rational structure-based drug design. This contribution delineates this strategy to minimize the potential for reactive metabolite formation of clinical candidates during preclinical drug optimization, exemplified by the experience at Roche over the past decade...
November 26, 2016: Drug Discovery Today
https://www.readbyqxmd.com/read/27903232/solution-structure-and-expression-profile-of-an-insect-cytokine-manduca-sexta-stress-response-peptide-2
#9
Lynn Goss Schrag, Xiaolong Cao, Alvaro Ivan Herrera, Yang Wang, Haobo Jiang, Om Prakash
Manduca sexta stress response peptide-2 (SRP2) is predicted to be a 25-residue peptide (FGVKDGKCPSGRVRRLGICVPDDDY), which may function as an insect cytokine to regulate immune responses. Produced as an inactive precursor, endogenous proSRP2 is probably converted to active SRP2 by limited proteolysis in response to invading pathogens, along with prophenoloxidase and pro-Spätzle activation. In addition to immunity, SRP2 may control head morphogenesis or other developmental processes in the lepidopteran insect...
November 21, 2016: Protein and Peptide Letters
https://www.readbyqxmd.com/read/27902924/simple-mechanisms-of-early-life-simulation-model-on-the-origin-of-semi-cells
#10
Adrian Klein, Martin Bock, Wolfgang Alt
The development of first cellular structures played an important role in the early evolution of life. Early evolution of life probably took place on a molecular level in a reactive environment. The iron-sulfur theory postulates the formation of cell-like structures on catalytic surfaces. Experiments show that H2S together with FeS and other metallic centers drive auto-catalytic surface reactions, in which organic molecules such as pyruvic and amino acids occur. It is questionable which mechanisms are needed to form cell-like structures under these conditions...
November 27, 2016: Bio Systems
https://www.readbyqxmd.com/read/27902479/identification-of-a-novel-polo-like-kinase-1-inhibitor-that-specifically-blocks-the-functions-of-polo-box-domain
#11
Yunyu Chen, Jing Zhang, Dongsheng Li, Jiandong Jiang, Yanchang Wang, Shuyi Si
Polo-like kinase 1 (Plk1) is a promising target for cancer therapy due to its essential role in cell division. In addition to a highly conserved kinase domain, Plk1 also contains a Polo-Box domain (PBD), which is essential for Plk1's subcellular localization and mitotic functions. We adopted a fluorescence polarization assay and identified a new Plk1 PBD inhibitor T521 from a small-molecule compound library. T521 specifically inhibits the PBD of Plk1, but not those of Plk2-3. T521 exhibits covalent binding to some lysine residues of Plk1 PBD, which causes significant changes in the secondary structure of Plk1 PBD...
November 25, 2016: Oncotarget
https://www.readbyqxmd.com/read/27900812/spontaneous-assembly-of-an-organic-inorganic-nucleic-acid-z-dna-double-helix-structure
#12
Vladislav Kulikov, Naomi A B Johnson, Andrew J Surman, Marie Hutin, Sharon M Kelly, Mohammed Hezwani, De-Liang Long, Gerd Meyer, Leroy Cronin
Herein, we report a hybrid polyoxometalate organic-inorganic compound, Na2 [(HGMP)2 Mo5 O15 ]⋅7 H2 O (1; where GMP=guanosine monophosphate), which spontaneously assembles into a structure with dimensions that are strikingly similar to those of the naturally occurring left-handed Z-form of DNA. The helical parameters in the crystal structure of the new compound, such as rise per turn and helical twist per dimer, are nearly identical to this DNA conformation, allowing a close comparison of the two structures...
November 30, 2016: Angewandte Chemie
https://www.readbyqxmd.com/read/27898513/inhibition-of-plasmin-generation-in-plasma-by-heparin-low-molecular-weight-heparin-and-a-covalent-antithrombin-heparin-complex
#13
Gabriela M T Chang, Helen M Atkinson, Leslie R Berry, Anthony K C Chan
The clinical limitations of unfractionated heparin (UFH) and low molecular weight heparin (LMWH) led to the development of an antithrombin-heparin covalent complex (ATH), which displays superior anticoagulant abilities compared with UFH. A recent study investigating its interaction with fibrinolysis showed that ATH inhibited free and fibrin bound plasmin and decreased plasmin generation on fibrin clots. These studies were conducted using purified components and did not elucidate the interaction of ATH with plasmin in the presence of its natural inhibitors α2-antiplasmin (α2-AP) and α2-macroglobulin (α2-M)...
November 24, 2016: Blood Coagulation & Fibrinolysis: An International Journal in Haemostasis and Thrombosis
https://www.readbyqxmd.com/read/27898334/relative-contribution-of-ammonia-oxidizing-bacteria-and-other-members-of-nitrifying-activated-sludge-communities-to-micropollutant-biotransformation
#14
Yujie Men, Stefan Achermann, Damian E Helbling, David R Johnson, Kathrin Fenner
Improved micropollutant (MP) biotransformation during biological wastewater treatment has been associated with high ammonia oxidation activities, suggesting co-metabolic biotransformation by ammonia oxidizing bacteria as an underlying mechanism. The goal of this study was to clarify the contribution of ammonia oxidizing bacteria to increased MP degradation in nitrifying activated sludge (NAS) communities using a series of inhibition experiments. To this end, we treated a NAS community with two different ammonia oxidation inhibitors, namely octyne (OCT), a mechanistic inhibitor that covalently binds to ammonia monooxygenases, and allylthiourea (ATU), a copper chelator that depletes copper ions from the active center of ammonia monooxygenases...
November 22, 2016: Water Research
https://www.readbyqxmd.com/read/27898006/immobilization-of-neutral-protease-from-bacillus-subtilis-for-regioselective-hydrolysis-of-acetylated-nucleosides-application-to-capecitabine-synthesis
#15
Teodora Bavaro, Giulia Cattaneo, Immacolata Serra, Ilaria Benucci, Massimo Pregnolato, Marco Terreni
This paper describes the immobilization of the neutral protease from Bacillus subtilis and its application in the regioselective hydrolysis of acetylated nucleosides, including building blocks useful for the preparation of anticancer products. Regarding the immobilization study, different results have been obtained depending on the immobilization procedure. Epoxy hydrophobic carriers gave a poorly stable derivative that released almost 50% of the immobilized protein under the required reaction conditions. On the contrary, covalent immobilization on a differently activated hydrophilic carrier (agarose) resulted in very stable enzyme derivatives...
November 25, 2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/27897433/affinity-chromatography-matrices-for-depletion-and-purification-of-casein-glycomacropeptide-from-bovine-whey
#16
María F Baieli, Nicolás Urtasun, María J Martinez, Daniela B Hirsch, Ana M R Pilosof, María V Miranda, Osvaldo Cascone, Federico J Wolman
Casein glycomacropeptide (CMP) is a 64- amino acid peptide found in cheese whey, which is released after κ-casein specific cleavage by chymosin. CMP lacks aromatic amino acids, a characteristic that makes it usable as a nutritional supplement for people with phenylketonuria. CMP consists of two nonglycosylated isoforms (aCMP A and aCMP B) and its different glycosylated forms (gCMP A and gCMP B). The most predominant carbohydrate of gCMP is N-acetylneuraminic acid (sialic acid). Here, we developed a CMP purification process based on the affinity of sialic acid for wheat germ agglutinin (WGA)...
November 7, 2016: Biotechnology Progress
https://www.readbyqxmd.com/read/27897389/new-insights-into-the-difference-between-rotaxane-and-pseudorotaxane
#17
He-Lue Sun, Heng-Yi Zhang, Zhen Dai, Xu Han, Yu Liu
Rotaxane and pseudorotaxane are two sorts of different mechanically interlocked molecular architectures, and there is obvious topological difference and boundary between them. In this work, a "suggested [2]rotaxane 1α-CD" was constructed based on an axle molecule 1 bearing two terminal ferrocene groups and a wheel component α-cyclodextrin (α-CD), but the result obtained indicated that the ferrocene group cannot prevent α-CD dethreading under UV irradiation. That is, 1α-CD is just a pseudo[2]rotaxane...
November 29, 2016: Chemistry, An Asian Journal
https://www.readbyqxmd.com/read/27897383/photoswitchable-and-watersoluble-fluorescence-nano-aggregates-based-on-diarylethene-dansyl-dyad-and-liposome
#18
Hongbo Cheng, Pin Ma, Yanan Wang, Guofei Hu, Shibi Fang, Yanyan Fang, Yuan Lin
In this work, a unique approach is developed to generate photoswitchable and watersoluble fluorescence nano-aggregates. Initially, a new light-controlled diarylethene-dansyl dyad DAEs 1 is formed by two dansyl fluorophores covalently linked to a symmetrical dithienylethene backbone, whose photophysical properties can be excellent reversibly switched by optical stimuli. Subsequently, the water-insolubility of molecular switch DAEs 1 is overcome by incorporating it into the bilayer of liposome DPPC (1,2-dihexadecanoyl-sn-glycero-3-phosphocholine) in water...
November 29, 2016: Chemistry, An Asian Journal
https://www.readbyqxmd.com/read/27897377/a-sequential-recognition-for-zinc-ion-and-pyrophosphate-based-on-a-terpyridine-derivative-functionalized-single-nanochannel
#19
Yuqi Zhang, Ru Zhou, Zhiju Zhao, Xiang-Yu Kong, Ganhua Xie, Qian Liu, Pei Li, Zhen Zhang, Kai Xiao, Zhengping Liu, Liping Wen, Lei Jiang
A highly selective recognition system for Zinc (II) ion and pyrophosphate (PPi) has been constructed using a N'-(4-((2,2':6',2″-terpyridine)-4-yl)benzyl)ethane-1,2-diamine (TPYD) functionalized single conical nanochannel by covalent attachment. The immobilized TPYD acted as a specific coordination site for Zn2+ to form TPYD-Zn2+ complexes over other metal ions, and subsequently, the resulted Zn2+-coordinated nanochannel could be employed as selective recognition elements for PPi ion based on the coordination reaction between hydroxyl oxygen of PPi and Zn2+...
November 29, 2016: Chemphyschem: a European Journal of Chemical Physics and Physical Chemistry
https://www.readbyqxmd.com/read/27897341/adaptive-self-assembly-behaviour-restrained-by-supramolecular-crystallization-and-molecular-recognition
#20
Seiji Shinkai, Bappaditya Roy, Takao Noguchi, Daisuke Yoshihara, Junji Sakamoto, Tatsuhiro Yamamoto
Recently, the supramolecular community is integrating different approaches to find converging ideas towards understanding the 'origin of life'. In this report, we have found an interesting adaptation trait, as like in Darwin's theory, in a bolaamphiphile molecule and established an environment friendly behaviour under non-covalent forces leading to evolve diverse assembly structures and interesting photo-physical properties. The perylene diimide (PDI)-based bolaamphiphile is used as a promising scaffold with great potential for the development of emerging supramolecular system...
November 29, 2016: Chemistry: a European Journal
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